Patch

Abstract

A Bisoprolol patch, wherein the skin penetration rate of Bisoprolol after 24 hours is 15 to 60% of the maximum skin penetration rate thereof, shows a little difference between the maximum level of the concentration in blood and the minimum level thereof in repeated administration and, therefore, scarcely exhibits side effects. Moreover, it achieves the quick development of the drug effect owing to the stabilization of the concentration in blood within a short time.

Description

[0001]This patent application is a divisional of U.S. application Ser. No. 11 / 814,840, filed Jul. 26, 2007, which is the U.S. National Stage of International Application No. PCT / JP2006 / 300419 filed Jan. 16, 2006, which claims the benefit of priority from Japanese Application No. 2005-024049 filed Jan. 31, 2005, each of which are herein incorporated by reference in their entirety.TECHNICAL FIELD[0002]The invention relates to a patch comprising Bisoprolol which is a β-blocker.BACKGROUND ART[0003]As administration methods for drugs, an oral administration using tablets, capsules, syrups and the like has been made in many drugs. However, in case of the oral administration, there were drawbacks that it lacked in duration of the effect, an unnecessary high blood concentration was recognized for a while after the administration, whereby a side effect occurred easily, and the like.[0004]Bisoprolol is high in β1-receptor selectivity and a β-blocker which does not have an intrinsic sympathomi...

AI Technical Summary

Benefits of technology

"The invention is a patch containing a drug called Bisoprolol and its salt. The patch has a specific ratio between the level of skin penetration of the drug and its maximum level in blood. This ratio ensures that the patch shows minimal side effects and a quick development of the drug effect with stable blood levels. The patch also causes minimal skin irritation. The invention also includes the use of specific polymers in the patch formulation to improve skin penetration and stability of the drug. The technical effect of the invention is a more effective and safe patch for the delivery of Bisoprolol."

Problems solved by technology

However, in case of the oral administration, there were drawbacks that it lacked in duration of the effect, an unnecessary high blood concentration was recognized for a while after the administration, whereby a side effect occurred easily, and the like.

Although Bisoprolol is relatively little in the effect to bronchus due to the high β1 selectivity, there are cases that symptoms such as bradycardia, dizziness and physical weariness occur, and there were problems in the point of stabilization of the concentration in blood and sustainability of the effect.

However, although this patch attained almost constant and stable skin penetration rate (FIG. 1 and FIG. 2 in patent document 1), there were inconveniences such as difficulty to obtain an effective blood concentration for therapy or necessity to take much time till the blood concentration when repeating administration was stabilized.

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